Global Patent Index - EP 0817782 B1

EP 0817782 B1 2002-09-25 - PHENYL DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS

Title (en)

PHENYL DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS

Title (de)

PHENYL DERIVATE UND IHRE VERWENDUNG ALS ENDOTHELIN REZEPTOR

Title (fr)

DERIVES DE PHENYLE UTILES COMME ANTAGONISTES DES RECEPTEURS DE L'ENDOTHELINE

Publication

EP 0817782 B1 (EN)

Application

EP 96910003 A

Priority

  • EP 9601237 W
  • GB 9506168 A
  • GB 9515591 A

Abstract (en)

[origin: WO9630358A1] Compounds of Formula (I), wherein R is a group Ar as defined hereinafter; R<1> is hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, X(CH2)pAr; or a methylenedioxy group attached to two adjacent ring carbon atoms; R<2> is -(CH2)xC(O)N(R<4>)S(O)yR<5>, -(CH2)xS(O)yN(R<4>)C(O)R<5>, -(CH2)xC(O)N(R<4>)C(O)R<5>, -(CH2)xS(O)yN(R<4>)S(O)yR<5>, -(CH2)xCO2R<4>, or tetrazol-5-yl optionally substituted by C1-6alkyl; R<3> is X(CH2)pAr or -X(CH2)pR<4> or a group of formula (a): Ar is a group of formula (b) or (c); or Ar is naphthyl, indolyl, pyridyl, thienyl, furyl, oxazolidinyl, oxazolyl, thiazolyl, isothiazolyl, pyrazolyl, triazolyl, tetrazolyl, imidazolyl, imidazolidinyl, thiazolidinyl, isoxazolyl, oxadiazolyl, thiadiazolyl, morpholinyl, piperidinyl, piperazinyl, pyrrolyle, or pyrimidyl; all of which may be unsubstituted or substituted by one or more R<7> or R<8> groups; A is C=O, or (C(R<4>)2)m; each B is independently -CH2- or -O-; and their pharmaceutically acceptable salts are endothelin antagonists and are useful e.g. for the treatment of renal failure, cerebrovascular disease and hypertension.

IPC 1-7 (main, further and additional classification)

C07D 317/60; A61K 31/36; A61K 31/41; C07D 317/64; C07D 403/12

IPC 8 full level (invention and additional information)

C07D 317/14 (2006.01); A61K 31/357 (2006.01); A61K 31/36 (2006.01); A61K 31/41 (2006.01); A61P 1/16 (2006.01); A61P 9/00 (2006.01); A61P 9/08 (2006.01); A61P 9/10 (2006.01); A61P 9/12 (2006.01); A61P 43/00 (2006.01); C07D 317/60 (2006.01); C07D 317/64 (2006.01); C07D 405/12 (2006.01)

CPC (invention and additional information)

C07D 317/60 (2013.01); C07D 317/64 (2013.01)

Designated contracting state (EPC)

BE CH DE DK FR GB IT LI NL

EPO simple patent family

WO 9630358 A1 19961003; AU 5333796 A 19961016; DE 69623941 D1 20021031; DE 69623941 T2 20030430; EP 0817782 A1 19980114; EP 0817782 B1 20020925; JP H11502530 A 19990302; US 6147111 A 20001114

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